MBM-55-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMBM-55Cat.No.:HY-101029CASNo.:2083622-09-5分⼦式:C₂₈H₂₇FN₆O₂分⼦量:498.55作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:125mg/mL(250.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0058mL10.0291mL20.0582mL5mM0.4012mL2.0058mL4.0116mL10mM0.2006mL1.0029mL2.0058mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性MBM-55有效的NIMA-relatedkinase2(Nek2)抑制剂，IC50值为1nM，其他激酶选择性的20倍甚⾄更⾼，除了RSK1(IC50=5.4nM)和DYRK1a(IC50=6.5nM)。MBM-55通过诱导细胞周期停滞和凋亡(apoptosis)抑制癌细胞的增殖。具有抗肿瘤活性，且对⼩⿏没有明显的毒性[1]。IC50&TargetIC50:1nM(Nek2),5.4nM(RSK1),6.5nM(DYRK1a),57nM(CHK1),91nM(GSK-3β),20nM(ABL),370nM(CDK2),441nM(CDK4),608nM(AKT1),5300nM(AuroraA)[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究MBM-55(compound42g)inhibitsMGC-803,HCT-116,Bel-7402cellsproliferationwithIC50sof0.53,0.84,7.13μM,respectively[1].MBM-55(0.5-1μM;24hours)inducesG2/Mphasearrestandaccumulationofcellswith>4NcontentinHCT-116cells[1].MBM-55(0.5-1μM;24hours)causescellapoptosisinaconcentration-dependentmannerinHCT-116cells[1].CellCycleAnalysis[1]CellLine:HCT-116cellsConcentration:0.5,1μMIncubationTime:24hoursResult:InducedG2/Mphasearrestandaccumulationofcellswith>4Ncontent.ApoptosisAnalysis[1]CellLine:HCT-116cellsConcentration:0.5,1μMIncubationTime:24hoursResult:Causedcellapoptosisinaconcentration-dependentmanner.体内研究MBM-55(20mg/kg;i.p.;twiceadayfor21days)exhibitsgoodantitumoractivityandawell-tolerateddosescheduleinnudemicebearingHCT-116xenografts[1].MBM-55(1.0mg/kg;i.v.)treatmentshowstheCL,Vss,T1/2,AUC0-t,andAUC0-∞valuesof33.3mL/min/kg,2.53L/kg,1.72hours,495ng/h/mLand507ng/h/mL,respectively.AnimalModel:FemaleBALB/cnu/numice(5-6weeks,bearingHCT-116xenografts)[1]Dosage:20mg/kgAdministration:Intraperitonealinjection;twiceadayfor21daysResult:Significantlysuppressedtumorgrowth.AnimalModel:MaleSpragueDawley(SD)rats[1]Dosage:1.0mg/kgAdministration:IVinjection(PharmacokineticAnalysis)Result:TheCL,Vss,T1/2,AUC0-t,andAUC0-∞valueswere33.3mL/min/kg,2.53L/kg,1.72hours,495ng/h/mLand507ng/h/mL,respectively.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].XiJB,etal.Structure-baseddesignandsynthesisofimidazo[1,2-a]pyridinederivativesasnovelandpotentNek2inhibitorswithinvitroandinvivoantitumoractivities.EurJMedChem.2017Jan27;126:1083-1106.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic